Synthesis of Tegafur by the Alkylation of 5-Fluorouracil under the Lewis Acid and Metal Salt-Free Conditions,Organic Process Research & Development

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Synthesis of Tegafur by the Alkylation of 5-Fluorouracil under the Lewis Acid and Metal Salt-Free Conditions
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2017-05-10 00:00:00 , DOI: 10.1021/acs.oprd.7b00103
Aleksandra Zasada ₁ , Ewa Mironiuk-Puchalska ₁ , Mariola Koszytkowska-Stawińska ₁

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A novel protocol for preparation of tegafur (a prodrug of 5-fluorouracil) is reported. The process involves the 1,8-diazabicycloundec-7-ene-mediated alkylation of 5-fluorouracil with 2-acetoxytetrahydrofuran at 90 °C, followed by treatment of the prepurified mixture of the alkylation products with aqueous ethanol at 70 °C. The yield of the two-step process is 72%.

中文翻译：

路易斯酸和无金属盐条件下5-氟尿嘧啶烷基化合成替加氟

报道了一种制备替加氟（5-氟尿嘧啶的前药）的新方案。该方法包括在90°C下用2-乙酰氧基四氢呋喃进行1，8-二氮杂双环十一烷基-7-烯介导的5-氟尿嘧啶的烷基化反应，然后在70°C下用乙醇水溶液处理烷基化产物的预纯化混合物。两步法的产率为72％。

更新日期：2017-05-17

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